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Class 548/503 - Nitrogen attached indirectly to ring carbon of the bicyclo ring system by acyclic nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached indirectly to ring
No. of patents: 179
Last issue date: 05/20/2008


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NumberTitleIssue Date
7375219Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p...
05/20/2008
7365090Substituted phenylindoles for the treatment of HIV
This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydro...
04/29/2008
7365091Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful fo...
04/29/2008
7259250C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
08/21/2007
7217706Propanolamine derivatives
This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympatho...
05/15/2007
7202383Compounds useful for modulating abnormal cell proliferation
There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1...
04/10/2007
7202268Derivatives of indole-3-carboxamide, preparation method thereof and application of same in therapeutics
The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3–C10 alkyl, a C5–C10 carbocyclic radi...
04/10/2007
7176322Calcium receptor modulating agents
The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and the...
02/13/2007
7157488N-(2-Arylethyl) benzylamines as antagonists of the 5-HTreceptor
The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invent...
01/02/2007
7138418Pentafluorobenzenesulfonamides and analogs
The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states...
11/21/2006
7126009Palladium catalyzed indolization of 2-bromo or chloroanilines
The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I)
10/24/2006
7122571Substituted hydrazones as inhibitors of cyclooxygenase-2
Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.
10/17/2006
7098307Neo-tryptophan
The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptid...
08/29/2006
7075582Methods for identifying and using MarR family polypeptide binding compounds
Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides. ...
07/11/2006
7071180Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2â€...
07/04/2006
7049308C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less th...
05/23/2006
7041697Antidepressant cycloalkylamine derivatives of 2,3-dihydro-1,4-benzodioxan
Compounds of the Formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorde...
05/09/2006
7026515Optically active amine derivatives and preparation process therefor
A readily available and inexpensive natural α-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula...
04/11/2006
6951881(1-substituted-indol-3-yl) alkylidenehydrazinecarboximidamide derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a disorder relating to or affected by the 5-HT6 receptor. ...
10/04/2005
6949556Acylated 1,2,3,4-tetrahydronaphthyl amines and their use as pharmaceutical agents
The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C a...
09/27/2005
6939889Quarternary ammonium compounds
Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans. ...
09/06/2005
6921805Neo-tryptophan
The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptid...
07/26/2005
69193541-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor ...
07/19/2005
6867200(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents ...
03/15/2005
6861444Bicyclic compounds
Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5
03/01/2005
6841563Aryloxy propanolamines for improving livestock production
Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group. R4 and R5 are independently —H, a C1-C4 straight chained or branched...
01/11/2005
6825352Preparation and use of ortho-sulfonamido arylhydroxamic acids as matrix metalloproteinase inhibitors
Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs. ...
11/30/2004
6803384Diaminopropionic acid derivatives
A compound of formula Id and pharmaceutically acceptable salts and esters thereof, wherein the substituent designations are as provided in the specification. Compounds of the invention are useful for treating reperfusi...
10/12/2004
6787535Indole derivatives with 5HT6 receptor affinity
This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, where...
09/07/2004
6765099Neo-tryptophan
The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptid...
07/20/2004
6750242Positive modulators of nicotinic receptor agonists
Compounds of Formula I wherein R1, R2, R3 and R4 are as defined in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing th...
06/15/2004
6716837Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with th...
04/06/2004
67100691-aryl- or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor. ...
03/23/2004
6710185Process for the preparation of cell proliferation inhibitors
The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors. ...
03/23/2004
6706751Dihydroindole and tetrahydroquinoline derivatives
The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are asso...
03/16/2004
6683101Bicyclic cyclohexylamines and their use as NMDA receptor antagonists
Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of the formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders...
01/27/2004
6583144Nitrogen-containing heterocyclic compounds and therapeutic agents for hyperlipidemia comprising the same
Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein ...
06/24/2003
6534535Inhibitors of factor Xa
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: ##STR1## are useful in vitro or in vivo for preventing or treating coagulation disorders....
03/18/2003
65093571-aryl or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor. ##STR1##...
01/21/2003
6503907Indole and dihydroindole derivatives
The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are ass...
01/07/2003
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